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The anticancer effect of a new pyrazole derivative, KI-10F (2-(4-(2-(4-(dimethylamino)phenyl)pyridin-4-yl)-5-(3-methoxy-5-methylphenyl)-1H-pyrazol‑1-yl) acetonitrile)•3.5HCl)was evaluated in human colon cancer cells. KI-10F strongly suppressed the growthof human colon cancer cells and induced apoptosis by increasing the proportionof sub-G1 presenting apoptotic cells as well as causing cell cycle arrest at theG2/M phase. Apoptosis by KI-10F was confirmed by observation of an increase inthe expression of cleaved caspase-3, caspase-8, caspase-9 and Bax, and the decreaseof Bcl-2. Decreased expression of HIF-1α and VEGF, and the inhibition of HUVECtube formation and migration showed that KI-10F effectively inhibited the angiogenesisprocess. Furthermore, in vivo study in a mouse xenograft model showed that KI-10Fproduced a stronger antitumor activity than 5-FU, a conventional anticancer drugprescribed for the treatment of colon cancer. The effects of KI-10F on tumor proliferation(PCNA), angiogenesis (CD34) and apoptosis (cleaved caspase-3) were evaluated byimmunohistochemistry using isolated tumor tissue samples. Taken together, ourresults demonstrated that KI-10F induces apoptosis and inhibits cell growth andangiogenesis both in vitro and in vivo. We suggest that KI-10F is an effectivechemotherapeutic candidate for use against colon cancer.

Anticancer effects of KI-10F: A novel compound affecting apoptosis, angiogenesis and cell growth in colon cancer